The Ginoide Hydrolipodystrophy (GHLD), commonly known as cellulite, occurs in 80-90% of the female population after the puberty period and comes from a metabolic modification in the cutaneous adipose tissue. Caffeine has been used in topical formulations due to its lipolytic action. We studied a nanoemulsion (F3) containing caffeine with two surfactants (oleth-3 and oleth-20) by emulsification method by phase inversion temperature inversion (PIT). The polydispersion indices (PDI) showed the reduced deviation of 0.1. The mean droplet size was ~ 40 nm. The evaluated constant of Ostwald, in the refrigerator condition was the most favorable during the stability test. In the In Raman spectroscopy assay, the caffeine bands found in F3 were compatible with those found in the caffeine solution (1337, 652.5 and 558.2 cm-1). There was no interaction of caffeine anhydrous with other ingredients in nanoemulsion. In the in vitro safety assay the result of 1.4 ranked the F3 as slightly irritating. In the natural membrane, cutaneous permeation test (human skin) permeate concentrations did not exceed the saturation concentration of the PBS buffer (48.96 µg/3 mL). The caffeine solution and F3 permeated statistically equal, but the nanoemulsion visually and sensorially improved the caffeine precipitation.

ABSTRACT Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids.

AbstractPassiflora alata Curtis, Passifloraceae, is a liana popularly known in Brazil as ‘maracujá-doce’ that has been used for treating different illnesses. Its leaves are described in the Brazilian Pharmacopoeia, but the gastroprotective activity has never been investigated. In the present study a freeze-dried crude 60% ethanol–water extract of P. alata aerial parts was prepared. Total flavonoid content, expressed as vitexin, was 0.67% ± 0.01. The hemolytic activity was 32 units for P. alata, using Saponin (Merck®) as reference. P. alata presented EC50 of 1061.2 ± 8.5 µg/ml in the 2,2-diphenyl-1-picryhydrazyl assay and 1076 ± 85 µmol Trolox/g in the Oxygen Radical Absorbance Capacity assay. P. alata, its solvent fractions and a P. alatananopreparation were investigated for gastroprotective activity. The test samples exhibited gastroprotective activity on HCl/ethanol induced gastric mucosal lesions in rats. P. alata at doses of 100, 200 and 400 mg/kg, using the necrotizing agent at 150 mmol/l, inhibited 100% of ulcer formation (compared to the negative control), while lansoprazole (30 mg/kg) 77%. When tested against a more concentrated necrotizing agent (300 mmol/l), fractions of P. alata at 100 mg/kg reduced 57% (n-hexane), 34% (ethyl acetate) and 72% (aqueous fraction) the ulcer formation. In this assay, lansoprazole (30 mg/kg) inhibited 47%. When encapsulated, P. alata inhibited ulcer formation at 55%, 94% and 90% for dosages of 25, 50 and 100 mg/kg. These results suggest the potential use of P. alata as a gastroprotective herbal medicine.